Novel peptide agonists of GLP-1 activity

a peptide agonist and activity technology, applied in the field of new peptide agonists of glp-1 activity, can solve the problem of short half-life of glp-1, and achieve the effect of stable and effective, low blood glucose levels, and reduced glp-1 activity

Inactive Publication Date: 2004-06-03
ZEALAND PHARM AS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0012] There is a need for compounds that lower blood glucose levels in mammals, and are stable and effective. Therefore, it is an objective of the invention to provide novel compounds that lower blood glucose levels in mammals. Ideally, these should be effective when administered orally. It is a further object of the invention to provide novel peptide agonists of GLP-1 activity and / or exendin-4 activity. It is a still further purpose of the invention to provide peptide agonists of GLP-1 activity and / or exendin-4 activity having an increased half-life and / or a decreased clearance.
[0021] The peptide X is further characterised in being effective in improving glucose tolerance in a diabetic mammal.

Problems solved by technology

However, a major pharmacological problem with native GLP-1 is its short half-life.

Method used

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  • Novel peptide agonists of GLP-1 activity
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  • Novel peptide agonists of GLP-1 activity

Examples

Experimental program
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Effect test

examples

[0186] Peptide Synthesis, General Procedures

[0187] Apparatus and Synthetic Strategy

[0188] Peptides are synthesized batchwise in a polyethylene vessel equipped with a polypropylene filter for filtration using 9-fluorenylmethyloxycarbonyl (Fmoc) as the N-.alpha.-amino protecting group and suitable common protection groups for side-chain functionalities (Dryland et al., 1986, J. Chem. Soc., Perkin Trans. 1:125-137).

[0189] Solvents

[0190] Solvent DMF (N,N-dimethylformamide, Riedel de-Hen, Germany) is purified by passing it through a column packed with a strong cation exchange resin (Lewatit S 100 MB / H strong acid, Bayer AG Leverkusen, Germany) and analysed for free amines prior to use by addition of 3,4-dihydro-3-hydroxy-4-oxo-1,2,3-benzotriazine (Dhbt-OH) giving rise to a yellow color (Dhbt-O-anion) if free amines are present. Solvent DCM (dichloromethane, analytical grade, Riedel de-Hen, Germany) is used directly without purification. THF (tetrahydrofuran, analytical grade, Riedel de-H...

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Abstract

Novel peptide agonists of GLP-1 activity useful for lowering blood glucose levels. The novel peptides comprise variants of the GLP-1 or the exendin-4 polypeptide sequence and are pharmacologically active and stable. These peptides are useful in the treatment of diseases that benefit from regulation of excess levels of blood glucose and / or regulation of gastric emptying, such as diabetes and eating disorders.

Description

[0001] The present invention relates to novel peptide agonists of GLP-1 activity. More specifically the invention relates to novel peptides that lower blood glucose levels comprising variants of the exendin-4 polypeptide sequence and peptide conjugates comprising variants of the GLP-1 or the exendin-4 polypeptide sequences which are pharmacologically active and stable, and as agonists of GLP-1 activity are useful in the treament of diseases that benefit from regulation of excess levels of blood glucose and / or regulation of gastric emptying, such as diabetes and eating disorders. The present invention also relates to methods of preparing said novel peptides, a composition, e.g., a pharmaceutical composition, comprising a peptide of the invention and a physiologically acceptable carrier, to said peptide for use in therapy, a method of treating a disorder and to the use of said peptide for the manufacture of a pharmaceutical composition for use in therapy.[0002] A number of hormones th...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61KA61K38/00A61K47/48A61PC07KC07K14/575C07K14/605
CPCC07K14/57563A61K47/48238C07K14/605A61K38/00A61K38/26A61K47/62A61P3/04A61P3/10
Inventor LARSEN, BJARNE DUEMIKKELSEN, JENS DAMSGAARDNEVE, SOREN
Owner ZEALAND PHARM AS
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